1. Field of the Invention
The present invention relates generally to the use of glycopyrronium bromide, derivatives and/or isomers thereof in combination with one or more specified active substances and/or in a specified form in cosmetic preparations, in particular deodorant/antiperspirant preparations.
2. Discussion of Background Information
Human beings have two types of sweat glands. The eccrine sweat glands secrete mainly salt and water and do not usually contribute to the development of odors. The apocrine sweat glands are responsible for odor: they secrete fatty acids, cholesterols and other compounds. These substances are decomposed on the skin by bacteria, the break-down products producing the typical odor of sweat.
In order to suppress sweat odor over a longer period, the use of cosmetic preparations is indispensable. The customary cosmetic deodorants are based on different principles, which can also be combined: on the one hand active deodorant ingredients are used, which suppress the growth of the bacteria causing the sweat odor. These germination inhibiting (bacteriostatic) agents include, e.g., triclosan, chlorhexidine or the naturally occurring compounds such as farnesol and phenoxyethanol.
On the other hand, antiperspirants are used, which prevent sweat secretion by blocking the sweat gland outlets. In by far the most antiperspirants, the formation of sweat can be reduced through astringents—primarily aluminum salts such as aluminum hydroxychloride (aluchlorohydrate) or aluminum/zirconium salts.
The combination of astringents with antimicrobially active substances in one and the same composition is also customary. Furthermore, perfumes are used to cover the smell of sweat.
One disadvantage with the use of aluminum chlorohydrate is, e.g., that residues can discolor clothing in an unpleasant manner and the low pH value (acidic) of the cosmetic preparation negatively affects the biological balance of the skin.
In addition to the liquid deodorants, such as atomizers and roll-ons, solid preparations, e.g., deodorant sticks, powder, powder sprays, feminine hygiene agents, etc. are known and common.
The following prerequisites are associated with a satisfactory deodorant/antiperspirant agent, preferably only deodorants, the realization of which prerequisites represents the object of the present invention: 1) protection of the natural biology of the skin, 2) neutral scent, 3) effectiveness only with regard to deodorizing, i.e., only the avoidance and/or elimination of body odor 4) avoidance of the formation of resistant strains of bacteria 5) avoidance of the accumulation of the active agents on the skin 6) harmless in the case of overdosing or other unintended use 7) good cosmetic application 8) ease of use (e.g., as a liquid) and universal application in various cosmetic and external preparations 9) excellent tolerance by the skin and mucous membranes 10) use of environmentally friendly substances.
Glycopyrronium bromide (international nonproprietary name for (±)-(R*)-3-[(S*)-(cyclopentyl hydroxyphenylacetoxy]-1,1-dimethylpyrrolidiniumbromide) is an anticholinergic and spasmolytic known since 1960. It is referred to as “glycopyrrolate” chiefly in English usage, and is characterized by the following chemical structure:

Glycopyrrolate exhibits no or only slight antimicrobial effectiveness.
In the prior art it is based primarily on the use of glycopyrrolate-containing compositions for treating pathological sweating, such as primary or secondary hyperhidrosis, gustatory sweating (Frey's Syndrome).
Anaesthesia, 1983, Volume 38, pages 1195-1204, describes the use of glycopyrrolate in anesthesia. An overview is provided of the pharmacological aspects of glycopyrrolate, the anticholinergic properties and the suitability for reducing sweat gland activity being mentioned.
L. V. Allen, “Topical Agent Stops Facial Sweating,” Pharmacist, July 1998, discloses a glycopyrrolate and other pharmaceutical/cosmetic auxiliaries containing formulations for treating gustatory sweating and for treating Frey's Syndrome.
C. L. Hays et al., “The Frey Syndrome: A Simple, Effective Treatment,” Otolaryngol Head Neck Surg. 1982, 90, 419-425, describes a clinical comparative study on the topical treatment of gustatory sweating (Frey's Syndrome) with scopolamine and glycopyrrolate. This deals with pathological sweating. Based on the action mechanism of glycopyrrolate, it is disclosed that glycopyrrolate blocks the nerve stimulus of the skin's sweat cells that leads to primary sweat formation, and thereby exhibits fewer side effects than scopolamine, since as a quarternary ammonium compound it does not pass through the blood-brain barrier and penetrates biological membranes more slowly.
WO03/026585 describes the use of glycopyrronium bromide to inhibit eccrine perspiration in humans—although the effect of glycopyrronium bromide and its use against hyperhidrosis has been known for much longer.
WO-A-01/08681 discloses the treatment of a number of pathological conditions with compositions based on glycopyrrolate, a special anticholinergic amine. The conditions include gustatory sweating and “Frey's Syndrome,” which is understood to mean increased sweat formation in the auriculotemporal area, which can be triggered by local irritation and by certain foods. In addition hyperhidrosis (increased sweat secretion) is mentioned. Formulations are disclosed, which are suitable for topical application to the skin, such as ointments, creams, gels and pastes, and which a pharmaceutically tolerated carrier.
U.S. Pat. No. 6,433,033 discloses compositions containing 0.25 to 6% by weight, in particular 0.5 to 4% by weight glycopyrrolate together with other pharmaceutically acceptable constituents. This composition is used to treat hyperhidrosis and is applied topically.
WO-A-03/011340 discloses a pharmaceutical formulation containing glycopyrrolate or salts or derivatives thereof, in a quantity between 0.05 and 20% by weight and also a vehicle such as a gel and/or colloidal carrier system. The glycopyrrolate formulations are applied topically to treat hyperhidrosis.